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Ligand-Gated Ion Channels Overview

Jun 19, 2025

Overview

This lecture explains ligand-gated ion channels, focusing on how they function as membrane receptors to convert chemical signals into electrical responses in cells.

Types of Membrane Receptors

  • Three main membrane receptor categories: ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked receptors.
  • This lecture focuses on ligand-gated ion channels (also called ion channel-linked receptors).

Ligand-Gated Ion Channels: Structure and Function

  • Ligand-gated ion channels are transmembrane proteins that open or close when a ligand binds.
  • Commonly found in excitable cells like neurons because they enable rapid cellular responses to stimuli.
  • These channels have a specific site (allosteric site) where the ligand binds, often away from the actual channel pore.
  • Binding at the allosteric site causes a conformational change, opening the channel for ions to pass through.
  • Ligand binding is specific, following the lock and key or induced fit model.
  • Multiple ligand-binding sites can exist on a single channel protein.

Ion Flow and Cellular Response

  • When the channel opens, ions (e.g., potassium, sodium, chloride, calcium) rapidly move across the membrane.
  • This ion movement causes a change in the electrical properties of the cell, resulting in an intracellular electrical signal.
  • The process converts an extracellular chemical signal into an intracellular electrical response, enabling fast cellular actions.

Binding Site Location and Variability

  • Most ligand-binding sites are on the extracellular side of the membrane, as membrane receptors primarily detect external signals.
  • Rarely, ligand-binding may occur inside the cell.

Distinguishing from Other Ion Channels

  • Ligand-gated ion channels are not the same as voltage-gated ion channels, which open in response to membrane potential changes.
  • Ligand-gated channels are also different from stretch-activated ion channels, which respond to membrane deformation.

Key Terms & Definitions

  • Ligand-gated ion channel — A membrane protein that opens or closes in response to binding a chemical signal (ligand).
  • Ligand — A chemical messenger that binds to a receptor or channel.
  • Allosteric site — A site on a protein where a molecule binds and induces a functional change at a different site.
  • Transmembrane protein — A protein spanning the cell membrane, often acting as a channel or receptor.
  • Voltage-gated ion channel — A channel that responds to changes in membrane potential.
  • Stretch-activated ion channel — A channel that responds to physical deformation of the cell membrane.

Action Items / Next Steps

  • Review the differences between ligand-gated, voltage-gated, and stretch-activated ion channels.
  • Understand examples of ions (Na+, K+, Ca2+, Cl-) involved in these channels for next class.